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大鼠离体精囊节后α-肾上腺素能受体的药理学特性

Pharmacological characterization of the postjunctional alpha-adrenoceptors of the rat isolated seminal vesicle.

作者信息

Sharif S I, Gokhale S D, Chandranath S I

机构信息

Department of Pharmacology, Faculty of Medicine, Al-Arab Medical University, Benghazi, Libya.

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1990 May;341(5):425-31. doi: 10.1007/BF00176335.

Abstract

In an attempt to define the pharmacological characteristics of the postjunctional alpha-adrenoceptors of the rat seminal vesicle, responses to certain phenylethanolamine and imidazoline agonists were investigated, in vitro, under experimental conditions outlined by Furchgott (1972), using alpha 1-selective, non-selective and alpha 2-selective adrenoceptor antagonists. Adrenaline (ADR), noradrenaline (NA) and phenylephrine (PE) produced concentration-dependent contractions. In many experiments the concentration-response (C-R) curves had a distinct "shoulder" at the level of 60-80% of the maximum response (Emax), a situation reminiscent of the rat anococcygeus muscle and the rat basilar artery. The relative potencies of ADR:NA:PE, derived from their EC50 values, were 4.07:1:0.26. In contrast clonidine, oxymetazoline and naphazoline failed to contract the tissue even in concentrations up to 1 X 10(-3) M. In fact the imidazoline derivatives prevented responses to the phenylethanolamines. The antagonist action of clonidine, against phenylephrine, was studied in detail. Prazosin, phentolamine, yohimbine, corynanthine and clonidine all caused a rightward displacement of the C-R curves for NA without depressing Emax. The Arunlakshana and Schild plots of the data were linear and had slopes not significantly different from unity. The pA2 estimates obtained were 9.17 (9.13-9.21) for prazosin, 8.58 (8.07-9.09) for phentolamine, 6.70 (6.44-6.98) for yohimbine and 7.05 (6.81-7.30) for corynanthine. Clonidine had a pA2 value of 6.60 (6.55-6.67) against phenylephrine. On the basis of results obtained with antagonists, the postjunctional alpha-adrenoceptors of the rat seminal vesicle could be firmly placed in the gross category of "alpha 1".(ABSTRACT TRUNCATED AT 250 WORDS)

摘要

为了明确大鼠精囊节后α-肾上腺素能受体的药理学特性,在弗奇戈特(1972年)概述的实验条件下,于体外研究了对某些苯乙醇胺和咪唑啉激动剂的反应,使用α1选择性、非选择性和α2选择性肾上腺素能受体拮抗剂。肾上腺素(ADR)、去甲肾上腺素(NA)和去氧肾上腺素(PE)产生浓度依赖性收缩。在许多实验中,浓度-反应(C-R)曲线在最大反应(Emax)的60-80%水平处有明显的“肩部”,这种情况类似于大鼠肛门尾骨肌和大鼠基底动脉。由其EC50值得出的ADR:NA:PE相对效价为4.07:1:0.26。相比之下,可乐定、羟甲唑啉和萘甲唑啉即使在浓度高达1×10(-3) M时也未能使组织收缩。实际上,咪唑啉衍生物可阻断对苯乙醇胺的反应。详细研究了可乐定对去氧肾上腺素的拮抗作用。哌唑嗪、酚妥拉明、育亨宾、柯楠碱和可乐定均使NA的C-R曲线向右移位,而不降低Emax。数据的阿伦拉克沙纳和希尔德图呈线性,斜率与1无显著差异。哌唑嗪的pA2估计值为9.17(9.13-9.21),酚妥拉明为8.58(8.07-9.09),育亨宾为6.70(6.44-6.98),柯楠碱为7.05(6.81-7.30)。可乐定对去氧肾上腺素的pA2值为6.60(6.55-6.67)。根据拮抗剂的实验结果,大鼠精囊节后α-肾上腺素能受体可明确归为“α1”大类。(摘要截短于250字)

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